Emopamil Binding Protein

Emopamil Binding Protein (EBP) is a membrane-bound cholesterol biosynthetic enzyme involved in the key steps of cholesterol synthesis and a target for neuroprotective agents. It belongs to the extended EBP superfamily. Emopamil Binding Protein is mainly localized in the endoplasmic reticulum membrane and widely expressed in various tissues, especially the liver. EBP can bind to chemotherapeutic drugs, reducing their effectiveness and leading to tumor resistance.

References:

[1]. Emopamil. Pharmacology, Toxicology and Pharmaceutical Science. Sciencedirect.

[2]. Silve S, et al. Emopamil-binding protein, a mammalian protein that binds a series of structurally diverse neuroprotective agents, exhibits delta8-delta7 sterol isomerase activity in yeast. J Biol Chem. 1996 Sep 13;271(37):22434-40. [Content Brief]

[3]. Reardon D A, et al. DSP-0390, an oral emopamil binding protein (EBP) inhibitor, in patients with recurrent high-grade glioma: A first-in-human, phase 1 study[J]. 2022.

Emopamil Binding Protein Inhibitors (3)

Emopamil Binding Protein Related Products (3):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-164561

TASIN-30	Inhibitor	99.96%
TASIN-30 is a selective EBP inhibitor with an EC₅₀ of 0.097 μM. TASIN-30 blocks the production of 7-dehydrocholesterol (7-DHC) and downstream cholesterol biosynthesis processes. TASIN-30 depletes downstream sterols, disrupts the integrity of lipid rafts in tumor cells, accelerates intracellular cholesterol consumption, and inhibits tumor cell proliferation. TASIN-30 induces ferroptosis and apoptosis by reducing 7-DHC levels and increasing phospholipid peroxidation. TASIN-30 achieves tumor suppression in nude mice with osteosarcoma. TASIN-30 can be used in cancer-related research such as colorectal cancer and osteosarcoma.

HY-162351

EBP-IN-1	Inhibitor	99.77%
EBP-IN-1 is an orally active, blood-brain barrier-permeable inhibitor of emopamil binding protein (EBP). EBP-IN-1 has an IC₅₀ of 8.2 μM against human ERG potassium channels (in CHO background). By inhibiting the sterol isomerase activity of EBP, EBP-IN-1 causes the accumulation of Zymostenol (HY-113345), and exhibits strong target binding in the brain after repeated administration in rodents. EBP-IN-1 also promotes oligodendrocyte formation in human cortical organoids and can be used in research related to multiple sclerosis.

HY-157828

DSP-0390	Inhibitor
DSP-0390 is an orally effective inhibitor of Emopamil-binding protein (EBP). DSP-0390 blocks the cholesterol de novo synthesis pathway in tumor cells by inhibiting EBP, and demonstrates significant anti-tumor activity in an orthotopic xenograft model of glioblastoma (GBM). DSP-0390 can be used for the study of recurrent high-grade gliomas.

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